Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: possible confounding effects on in vivo and in vitro studies

…, SW Mascarella, S Runyon, L Brieaddy…

Index: McElhinny Jr., Charles J.; Lewin, Anita H.; Mascarella, S. Wayne; Runyon, Scott; Brieaddy, Lawrence; Carroll, F. Ivy Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 21 p. 6661 - 6664

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Citation Number: 32

Abstract

SB-334867 has been an important ligand for the study of the orexin 1 (OX1) receptor due to its high OX1/OX2 selectivity and bioavailability. This ligand however, contains a 2- methylbenzoxazole ring system which is known to undergo hydrolysis, particularly under acidic or basic conditions. The possibility that SB-334867 would be susceptible to significant hydrolysis was evaluated in various formulations and in the solid state. SB-334867 was ...